Menopause is very often associated with symptoms such as hot flushes. Such symptoms have a major negative impact on post-menopausal female life quality.
Estradiol (17-beta estradiol) is the most potent naturally occurring estrogen in mammals, in which it is formed by the ovary, placenta, testis, and possibly the adrenal cortex. Administering estradiol has proven effective for alleviating certain menopause-associated symptoms, in particular hot flushes. However, due to increasingly important patient safety requirements, it is highly desirable to provide compositions, methods and uses effective for alleviating such symptoms without overestimating the required therapeutic dose.
In Serum concentrations of 17beta-estradiol and estrone after multiple-dose administration of percutaneous estradiol gel in symptomatic menopausal women, Brennan J J, Lu Z, Whitman M, Stafiniak P, van der Hoop R G. Ther Drug Monit. 2001 April; 23(2):134-8, the authors used a hydro-alcoholic gel containing estradiol. They found that daily topical administration of a 0.75 mg dose of estradiol (1.25 g of said gel per day) resulted in an elevation in the serum estradiol level, reaching values compatible with a relief in vasomotor symptoms. Further, the authors indicated that a lower estradiol dose did not achieve similar serum levels, and thus was not expected to be consistently therapeutic in reducing vasomotor symptoms.